Serotonin receptor ligands

Muschamp, J.W. and Fong, P.P. (2001) Effects of the serotonin receptor ligand methiothepin on reproductive behavior of the freshwater snail Biomphalaria glabrata reduction of egg laying and induction of penile erection. Journal of Experimental Zoology 289, 202-207. 

Schieck C, Lee KS, Jones DW, et al. [123I]DOI a novel 5-HT2 serotonin receptor ligand for SPECT imaging 26th National Medicinal Chemistry Symposium, Richmond, VA, 1998. 

Prisinzano TP, Law H, Slassi A, MaClean N, Demchyshyn L, Glennon RA. QSAR studies on 2-benzylimidazoline analogs as h5-HT1D/1B serotonin receptor ligands. Med Chem Res 2001 10 309-317. 

Prisinzano T, Dukat M, Law H, et al. 2-(Anilino)imidazolines and 2-(benzyl)-imidazoline derivatives as /z5-HT1D serotonin receptor ligands. Bioorg Med Chem Lett 2004 14 4697-4699. 

Bondarev M, Iwamura T, Hynd D, et al. Aryloxyethylamines as h5-HT1D serotonin receptor ligands. Med Chem Res 1998 8 333-342. 

Pullagurla MR, Dukat M, Roth BL, Setola V, Glennon RA. 5-Azatryptamine analogs as / 5-HT6 serotonin receptor ligands. Med Chem Res 2005 14 1-18. 

Lee M, Rangisetty JB, Pullagurla M, et al. 1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. Bioorg Med Chem Lett 2005 15 1707-1711. 

Fig. 3.7 The serotonin receptor ligands 31 and 32 differ in their subtype selectivity. Whereas 31 is a highly selective 5-HT3 receptor ligand, compound 32 binds preferentially to the 5-HT4 receptor.

Figure 13.14 Projection of two promiscuous binders, Sertindole (primary target 5-HT2a, left) and Clozapine (primary target D4.2, right), onto the COBRA SOM. The distribution of known serotonin receptor ligands is shown in the left map, the distribution of known dopamine receptor ligands is shown in the right map. The colored areas of the two maps overlap, indicating similar activity of the compounds. Blue few compounds red many compounds crosses indicate unpopulated areas of pharmacophore space.

The 2-aminotetralin structure has proven to be a valuable structural base, not only for the development of dopamine receptor ligands, but also for the development of serotonin receptor and adrenoceptor ligands, as well as compounds that interact with melatonin receptors. The position of the aromatic hydroxyl group appeared to determine the kind of activity of the 2-aminotetralins, namely, 5- and 7-hydroxy-2-(N,N-di-Ai-propylamino)tetralin (5- and 7-OH-DPAT) are potent dopamine receptor ligands while 8-hydroxy-2-(N,N-di- -propylamino)tetralin (8-OH-DPAT) is a very potent and selective serotonin receptor ligand. 

At present, buspirone remains the only serotonin receptor ligand available for the treatment of anxiety The clinical development of several 5HT-1A agonists (ipsapirone, zalospi-rone, flesinoxan),5HT-2 antagonists (eplivan-serin, ritanserin), and mixed 5HT-1A agonist/... 

Abadi, A. H., Lankow, S., Hoefgen, B., Decker, M., Kassack, M. U., Lehmann, J. Dopamine/serotonin receptor ligands, part 111 synthesis and biological activities of 7, 7 -alkylene-te-6, 7, 8, 9, 14, 15-hexahydro-5H-benz[d]indolo[2, 3-g]azednes — application of the bivalent ligand approach to a novel type of dopamine receptor antagonist. Arch. Pharm. (Weinheim) 2002, 335, 367—373. 

PHE177 phenyl methylsulfamate serotonin receptor ligand 1998BMC6 1469... 

Complex molecules have been labeled with [ F]fluoride by direct aromatic nucleophilic substitution. The serotonin receptor ligands [ F]altanserin (Lemaire et al. 1991) O Fig. 42.10a) and the D2-like receptor ligand N-[ F]methylspiperone (Hamacher et al. 1986a) were successfully prepared by aromatic F-for-N02 and F-for-Cl exchange. 

The serotonin receptor ligand [ F]altanserin (a), the D2-like receptor ligand N-[ F] methylspiperone (b), the 5-HTia receptor antagonist p-[ F]MPPF (c), the CBl cannabinoid receptor ligand (d), and a F-labeled phenylthiophenyl derivative (e), specific for imaging of serotonin reuptake transporters (SERT)... 

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